EP3965886A1 - Nasal spray compositions and related treatment methods - Google Patents
Nasal spray compositions and related treatment methodsInfo
- Publication number
- EP3965886A1 EP3965886A1 EP20754134.3A EP20754134A EP3965886A1 EP 3965886 A1 EP3965886 A1 EP 3965886A1 EP 20754134 A EP20754134 A EP 20754134A EP 3965886 A1 EP3965886 A1 EP 3965886A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- composition
- mass
- concentration
- nasal spray
- nasal
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 134
- 238000000034 method Methods 0.000 title claims abstract description 41
- 239000007922 nasal spray Substances 0.000 title claims description 46
- 229940097496 nasal spray Drugs 0.000 title claims description 43
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims abstract description 28
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims abstract description 28
- 235000010447 xylitol Nutrition 0.000 claims abstract description 28
- 239000000811 xylitol Substances 0.000 claims abstract description 28
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims abstract description 28
- 229960002675 xylitol Drugs 0.000 claims abstract description 28
- 235000002961 Aloe barbadensis Nutrition 0.000 claims abstract description 17
- 244000186892 Aloe vera Species 0.000 claims abstract description 17
- 235000011399 aloe vera Nutrition 0.000 claims abstract description 17
- 239000000739 antihistaminic agent Substances 0.000 claims abstract description 13
- 239000003246 corticosteroid Substances 0.000 claims abstract description 11
- 229960000686 benzalkonium chloride Drugs 0.000 claims abstract description 5
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims abstract description 5
- 229940107702 grapefruit seed extract Drugs 0.000 claims abstract description 5
- 208000036142 Viral infection Diseases 0.000 claims abstract 4
- 206010022000 influenza Diseases 0.000 claims abstract 4
- 230000009385 viral infection Effects 0.000 claims abstract 4
- 206010020751 Hypersensitivity Diseases 0.000 claims description 24
- 230000007815 allergy Effects 0.000 claims description 24
- 208000026935 allergic disease Diseases 0.000 claims description 14
- SOYKEARSMXGVTM-UHFFFAOYSA-N chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 claims description 14
- 229960003291 chlorphenamine Drugs 0.000 claims description 14
- 229960000289 fluticasone propionate Drugs 0.000 claims description 14
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 claims description 14
- 239000007921 spray Substances 0.000 claims description 13
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims description 12
- 230000001387 anti-histamine Effects 0.000 claims description 12
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims description 7
- 229960000520 diphenhydramine Drugs 0.000 claims description 7
- 206010064948 Viral rhinitis Diseases 0.000 claims 3
- 206010051513 Viral sinusitis Diseases 0.000 claims 3
- 239000004615 ingredient Substances 0.000 abstract description 27
- 201000009890 sinusitis Diseases 0.000 abstract description 13
- 206010011224 Cough Diseases 0.000 abstract description 9
- 206010041232 sneezing Diseases 0.000 abstract description 4
- 206010039083 rhinitis Diseases 0.000 abstract description 3
- 229960001334 corticosteroids Drugs 0.000 abstract description 2
- 229940125715 antihistaminic agent Drugs 0.000 abstract 1
- 238000009472 formulation Methods 0.000 description 31
- 208000024891 symptom Diseases 0.000 description 17
- 230000008901 benefit Effects 0.000 description 11
- 238000001035 drying Methods 0.000 description 8
- 206010028740 Nasal dryness Diseases 0.000 description 6
- 230000003247 decreasing effect Effects 0.000 description 6
- 244000005700 microbiome Species 0.000 description 6
- 210000003928 nasal cavity Anatomy 0.000 description 6
- 210000002850 nasal mucosa Anatomy 0.000 description 6
- 206010009137 Chronic sinusitis Diseases 0.000 description 5
- 206010061218 Inflammation Diseases 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 208000027157 chronic rhinosinusitis Diseases 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 235000003599 food sweetener Nutrition 0.000 description 5
- 230000004054 inflammatory process Effects 0.000 description 5
- 239000003765 sweetening agent Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 206010001076 Acute sinusitis Diseases 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 230000001154 acute effect Effects 0.000 description 4
- -1 hexose sugar alcohol Chemical class 0.000 description 4
- 206010013911 Dysgeusia Diseases 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 235000013361 beverage Nutrition 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000007937 lozenge Substances 0.000 description 3
- 230000003020 moisturizing effect Effects 0.000 description 3
- 239000008213 purified water Substances 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- 239000000725 suspension Substances 0.000 description 3
- 239000003826 tablet Substances 0.000 description 3
- 235000013616 tea Nutrition 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- 239000012049 topical pharmaceutical composition Substances 0.000 description 3
- 208000035143 Bacterial infection Diseases 0.000 description 2
- SRBFZHDQGSBBOR-IOVATXLUSA-N D-xylopyranose Chemical compound O[C@@H]1COC(O)[C@H](O)[C@H]1O SRBFZHDQGSBBOR-IOVATXLUSA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 230000000844 anti-bacterial effect Effects 0.000 description 2
- 230000003466 anti-cipated effect Effects 0.000 description 2
- PYMYPHUHKUWMLA-UHFFFAOYSA-N arabinose Natural products OCC(O)C(O)C(O)C=O PYMYPHUHKUWMLA-UHFFFAOYSA-N 0.000 description 2
- 229960004335 azelastine hydrochloride Drugs 0.000 description 2
- YEJAJYAHJQIWNU-UHFFFAOYSA-N azelastine hydrochloride Chemical compound Cl.C1CN(C)CCCC1N1C(=O)C2=CC=CC=C2C(CC=2C=CC(Cl)=CC=2)=N1 YEJAJYAHJQIWNU-UHFFFAOYSA-N 0.000 description 2
- 230000001580 bacterial effect Effects 0.000 description 2
- 208000022362 bacterial infectious disease Diseases 0.000 description 2
- SRBFZHDQGSBBOR-UHFFFAOYSA-N beta-D-Pyranose-Lyxose Natural products OC1COC(O)C(O)C1O SRBFZHDQGSBBOR-UHFFFAOYSA-N 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 201000009240 nasopharyngitis Diseases 0.000 description 2
- 210000001331 nose Anatomy 0.000 description 2
- 150000005846 sugar alcohols Chemical class 0.000 description 2
- 230000002195 synergetic effect Effects 0.000 description 2
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 description 1
- 240000000560 Citrus x paradisi Species 0.000 description 1
- 229920000742 Cotton Polymers 0.000 description 1
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 description 1
- 239000004386 Erythritol Substances 0.000 description 1
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 1
- 208000005141 Otitis Diseases 0.000 description 1
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000000840 anti-viral effect Effects 0.000 description 1
- PYMYPHUHKUWMLA-WDCZJNDASA-N arabinose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)C=O PYMYPHUHKUWMLA-WDCZJNDASA-N 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 238000007664 blowing Methods 0.000 description 1
- 229960004436 budesonide Drugs 0.000 description 1
- 201000009151 chronic rhinitis Diseases 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000019258 ear infection Diseases 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 229960000676 flunisolide Drugs 0.000 description 1
- 229960001469 fluticasone furoate Drugs 0.000 description 1
- XTULMSXFIHGYFS-VLSRWLAYSA-N fluticasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(F)[C@@]4(C)C=CC(=O)C=C4[C@@H](F)C[C@H]3[C@@H]2C[C@H]1C)C(=O)SCF)C(=O)C1=CC=CO1 XTULMSXFIHGYFS-VLSRWLAYSA-N 0.000 description 1
- 230000002538 fungal effect Effects 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000007407 health benefit Effects 0.000 description 1
- 235000003642 hunger Nutrition 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 229960001361 ipratropium bromide Drugs 0.000 description 1
- KEWHKYJURDBRMN-ZEODDXGYSA-M ipratropium bromide hydrate Chemical compound O.[Br-].O([C@H]1C[C@H]2CC[C@@H](C1)[N@@+]2(C)C(C)C)C(=O)C(CO)C1=CC=CC=C1 KEWHKYJURDBRMN-ZEODDXGYSA-M 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 230000005923 long-lasting effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229960001664 mometasone Drugs 0.000 description 1
- QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 description 1
- 230000003843 mucus production Effects 0.000 description 1
- 244000052769 pathogen Species 0.000 description 1
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/75—Rutaceae (Rue family)
- A61K36/752—Citrus, e.g. lime, orange or lemon
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/88—Liliopsida (monocotyledons)
- A61K36/886—Aloeaceae (Aloe family), e.g. aloe vera
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/46—Ingredients of undetermined constitution or reaction products thereof, e.g. skin, bone, milk, cotton fibre, eggshell, oxgall or plant extracts
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
Definitions
- the composition may be provided in the form of a nasal spray and/or be delivered into a subject’s nasal and/or sinus passages.
- alternative embodiments and implementations may be made into suspensions, lozenges, tablets, capsules, topical formulations, and/or ingestible products, such as teas or other beverages, for example, or other liquid formulations that may be inserted into nasal passages other than in the form of a spray, such as drops.
- the method may comprise method for treating a cold or allergy condition and restoring nasal flora in a human, which method may comprise the steps of identifying a human subject having a cold or allergy condition and obtaining a nasal spray composition comprising chlorpheniramine in a concentration of between about 0.4% and about 10% by mass (in more preferred compositions, between about 0.4% and about 1 % by mass); xylitol in a concentration of between about 10% and about 15% by mass; and fluticasone propionate in a concentration of between about 0.03% and about 1.0% by mass.
- the nasal spray composition may then be delivered into the human subject’s nasal passages.
- the nasal spray composition may further comprise aloe vera.
- the aloe vera may be present in the composition in a concentration of between about 0.02% and about 2%.
- the nasal spray composition may further comprise at least one of benzalkonium chloride and grapefruit seed extract.
- the method may comprise identifying a human subject having a cold or allergy condition and obtaining a nasal spray
- the corticosteroid may comprise fluticasone propionate.
- the fluticasone propionate may be present in the composition in a concentration of between about 0.03% and about 1 % by mass.
- the nasal spray composition may further comprise aloe vera, which, in some such implementations, may be present in the composition in a concentration of between about 0.02% and about 2%.
- the composition may comprise an antihistamine, such as chlorpheniramine and/or diphenhydramine, which may be present in the composition in a concentration of between about 0.25% and about 10% (in more preferred compositions, between about 0.25% and about 4%) by mass.
- the composition may further comprise xylitol or another suitable non-hexose sugar alcohol. The xylitol and/or other sugar alcohol(s) may be present in the composition in a concentration of between about 5% and about 15% by mass.
- the xylitol and/or other sugar alcohol(s) may be present in the composition in a concentration of between about 10% and about 15% by mass.
- the composition may further comprise a corticosteroid, such as fluticasone propionate, which may be present in the composition in a concentration of between about 0.01 % and about 3% by mass.
- fluticasone propionate may be present in the composition in a concentration of between about 0.03% and about 1.0% by mass.
- the antihistamine may comprise chlorpheniramine.
- the chlorpheniramine may be present in the composition in a concentration of between about 0.4% and about 10% by mass (in more preferred compositions, between about 0.4 and about 1.0% by mass).
- Some embodiments may further comprise aloe vera, which preferably may be present in the composition in a concentration of between about 0.02% and about 3.0% by mass.
- the aloe vera may be present in the composition in a concentration of between about 0.05% and about 2.0% by mass.
- compositions that may be provided in nasal sprays and/or otherwise delivered into a subject’s nasal and/or sinus passages.
- the three formulations involved in this protocol include one that comprises an agent used for blocking mucus production, such as azelastine hydrochloride, one that comprises an agent used for nasal drying, such as ipratropium bromide, and one that comprises a corticosteroid for decreasing inflammation, such as flunisolide.
- these formulations are to be delivered with two sprays into each nostril twice daily for one month, after which the symptoms are reevaluated. If the symptoms have improved, the same regimen is continued for an additional two months, after which the dosage may be decreased to a single spray in each nostril twice daily, and then after an additional month to two months may be decreased again to a single spray in each nostril once daily.
- this protocol suffers from a number of drawbacks and disadvantages. For example, it is rather cumbersome and requires a patient to obtain and/or mix several different ingredients and/or formulations. This can also lead to confusion, misinterpretation, and/or misuse of the protocol guidelines, which can cause poor performance, overdose, and increase the risk of unwanted side effects. In addition, several of the formulations and/or ingredients are unpleasant in taste and/or smell and can cause an undesirable aftertaste (azelastine hydrochloride), also limiting its usefulness in treating children.
- the protocol is also rather expensive due to the various formulations involved. The protocol also has room for improvement in terms of efficacy. For example, the side effects can lead to dry nasal tissue, bacterial infections, and other side effects.
- the formulation will be available over the counter and will provide for treatment of sinusitis, rhinitis, and otitis in a single composition that may replace, and improve upon, a full regimen of other nasal sprays.
- compositions disclosed herein overcome many of these drawbacks and/or other drawbacks of the prior art by, in some preferred embodiments and/or treatment methods, combining the most desirable agents and concentrations into a single composition, preferably in the form of a nasal spray, and may include other ingredients for decreasing various side effects, such as xylitol or another non-hexose sugar alcohol, which may provide a number of benefits, such as inhibiting bacterial growth, fungal growth, decreasing undue nasal drying, enhancing anti-inflammatory benefits, and/or decreasing the unwanted aftertaste of the product.
- xylitol or another non-hexose sugar alcohol which may provide a number of benefits, such as inhibiting bacterial growth, fungal growth, decreasing undue nasal drying, enhancing anti-inflammatory benefits, and/or decreasing the unwanted aftertaste of the product.
- an antihistamine such as, in preferred embodiments, chlorpheniramine and/or diphenhydramine.
- chlorpheniramine or another suitable antihistamine may be present in the formulation in a concentration between about 2% and about 3% by mass.
- the concentration may be slightly less.
- the concentration of diphenhydramine may be between about 1 % and about 2% by mass.
- one or more corticosteroids or other intranasal steroids are included in the formulation.
- mometasone, fluticasone propionate, fluticasone furoate, triamcinolone acetonide, and/or budesonide glucocorticoid may be included.
- the corticosteroid may be present in the formulation in a concentration between about 0.01 and about 3% by mass, and may comprise, for example, fluticasone propionate.
- the fluticasone propionate may be present in a concentration of between about 0.03% and about 1 % by mass.
- the fluticasone propionate may be present in a
- xylitol or, alternatively, another non-hexose sugar alcohol, such as xylose, erythritol, ribose, and/or arabinose, may be included in the formulation.
- xylitol or another such ingredient may provide a number of benefits and may provide a synergistic effect with the other ingredients of the
- xylitol in particular has been shown to be very effective in moisturizing nasal passages and the like. Without being limited by theory, this is thought to occur because xylitol can create a hyper-osmotic solution that pulls moisture towards it from surrounding tissues without generated mucous.
- the combination of xylitol, or other similar compositions disclosed herein may result in a decrease in mucous production, potentially along with accompanying anti-bacterial and other health benefits associated with xylitol and/or other similar agents.
- Xylitol may also enhance the taste and/or reduce the negative smell/aftertaste issues commonly associated with prior art formulations. Moreover, by providing a sweetener that does not include sugar and serves as an active agent in the formulation, several benefits may be derived.
- xylitol acts as a sweetener
- xylitol enhances the ability of other agents to treat bacterial infections by actively starving the microorganisms causing the symptoms, rather than one that counteracts the active ingredients in a nasal spray or other treatment composition by feeding the microorganisms, or one that only passively starves the microorganisms by providing a sweetener that is not consumed by the more common oral and pharyngeal pathogens.
- compositions including xylitol may result in improved ability to treat various symptoms that may be caused by microorganisms (along with other not caused by microorganisms) and, more importantly, to fight the bacterial and/or other microorganisms behind these symptoms.
- xylitol or, alternatively, one of the other preferably non-hexose sugar alcohols disclosed herein, is present in a concentration of between about 5 and about 15% by mass. In more preferred formulations, xylitol may be present in a concentration of between about 10 and about 15% by mass. Although xylitol has been used as a sweetener in a variety of products, it should be noted that it is considered an active ingredient in the preferred formulations of the invention disclosed herein due to its moisturizing and/or antibacterial properties.
- More preferred formulations may include various other ingredients, such as aloe vera. Including aloe vera, preferably along with xylitol, may enhance the synergistic effects referenced elsewhere herein. More particularly, aloe vera may provide a soothing, moisturizing, and/or cooling effect that may increase user compliance and/or may heal irritated tissue, such as nasal and/or sinus passages in preferred embodiments, which may be caused by, for example, repeated nose wiping, sneezing, nose blowing, and the like. In preferred formulations, aloe vera is present in a concentration of between about 0.05 and about 3.0% by mass.
- grapefruit seed extract may be included in the formulation in an amount between about 0.01 and about 3% by mass.
- Glycerine if included, preferably ranges between about 0.05 and about 3% by mass.
- benzalkonium chloride which may be a suitable substitute for grapefruit seed extract, may be present in a concentration of between about 0.05 and about 0.2% by mass.
- the remainder of the formulation may comprise (preferably purified) water.
- purified water may be present in a range from about 80 to about 98% by mass. In some such formulations, the purified water may be present in a range from about 80 to about 90% by mass. In a more preferred
- water may be present in a concentration of about 87.5%.
- concentrations of the ingredients in these formulations may vary by around 5% from the concentrations provided herein.
- compositions preferably in the form of a nasal spray, for treating various symptoms associated with allergies, sinusitis, colds, and the like
- the composition may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below.
- concentrations may vary by, for example, by about 5% in certain alternative embodiments and related methods.
- one or more of these ingredients may be omitted and/or replaced with an alternative substantially similar ingredient in still other embodiments and related methods.
- the composition may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below. However, as mentioned above, these concentrations may vary by, for example, by about 5% in certain alternative embodiments and related methods. Similarly, one or more of these ingredients may be omitted and/or replaced with an alternative substantially similar ingredient in still other embodiments and related methods. compos on, e compos on may be delivered into a subject’s nasal cavity every twelve hours, preferably in the form of 1 - 2 sprays in each nostril.
- the present inventor has found that doing so is highly effective in drying the nasal mucosa, reducing inflammation, and/or restoring the natural, nasal flora. It can therefore be used to treat, for example, acute or chronic sinusitis and related conditions, including nasal drip, cough, and nasal dryness.
- compositions preferably in the form of a nasal spray, for treating various symptoms associated with allergies, sinusitis, colds, and the like, may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below. However, as mentioned above, these concentrations may vary by 5% in certain alternative
- the composition may be delivered into a subject’s nasal cavity every four to six hours, preferably in the form of 1 -2 sprays in each nostril.
- the present inventor has found that doing so is highly effective in drying the nasal mucosa, reducing inflammation, and/or restoring the natural, nasal flora. It can therefore be used to treat, for example, acute or chronic sinusitis and related conditions, including nasal drip, cough, and nasal dryness.
- compositions preferably in the form of a nasal spray, for treating various symptoms associated with allergies, sinusitis, colds, and the like, may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below. However, as mentioned above, these concentrations may vary by 5% in certain alternative
- c omposition may be delivered into a subject’s nasal cavity every four to six hours, preferably in the form of 1 -2 sprays in each nostril.
- the present inventor has found that doing so is highly effective in drying the nasal mucosa, reducing inflammation, and/or restoring the natural, nasal flora. It can therefore be used to treat, for example, acute or chronic sinusitis and related conditions, including nasal drip, cough, and nasal dryness.
- the composition may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below.
- the present inventor has found that doing so is highly effective in drying the nasal mucosa and/or restoring the natural, nasal flora. It can therefore be used to treat, for example, allergy and/or cold symptoms, including nasal drip, cough, and nasal dryness.
- the composition may be delivered into a subject’s nasal cavity every four to six hours, preferably in the form of 1 -2 sprays in each nostril.
- the present inventor has found that doing so is highly effective in drying the nasal mucosa and/or restoring the natural, nasal flora. It can therefore be used to treat, for example, allergy and/or cold symptoms, including nasal drip, cough, and nasal dryness.
- compositions preferably in the form of a nasal spray, for treating various symptoms associated with allergies, sinusitis, colds, and the like, may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below.
- compositions for treating various symptoms associated with allergies, sinusitis, colds, and the like, may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below.
- compositions preferably in the form of a nasal spray, for treating various symptoms associated with allergies, sinusitis, colds, and the like, may comprise the following ingredients in at least approximately the concentrations (by mass) presented in the chart below.
- compositions disclosed herein may be administered via liquid drops from a dropper, topically (in some cases using a cotton swab or the like), orally, via a mister or atomizer, and/or via any other suitable manner of administration.
- alternative compositions and treatment methods are contemplated in which the preferred nasal sprays may be replaced with
- Any methods disclosed herein may comprise one or more steps or actions for performing the described method.
- the method steps and/or actions may be
- any reference to“one embodiment,”“an embodiment,” or“the embodiment” means that a particular feature, structure, or characteristic described in connection with that embodiment is included in at least one embodiment.
- the quoted phrases, or variations thereof, as recited throughout this specification are not necessarily all referring to the same embodiment.
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US201962806364P | 2019-02-15 | 2019-02-15 | |
PCT/US2020/018430 WO2020168289A1 (en) | 2019-02-15 | 2020-02-14 | Nasal spray compositions and related treatment methods |
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EP3965886A1 true EP3965886A1 (en) | 2022-03-16 |
EP3965886A4 EP3965886A4 (en) | 2023-06-07 |
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US (1) | US20200261433A1 (en) |
EP (1) | EP3965886A4 (en) |
CA (1) | CA3159816A1 (en) |
WO (1) | WO2020168289A1 (en) |
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US5288492A (en) | 1992-11-13 | 1994-02-22 | Morris Michael A | Decongestant composition containing aloe vera |
WO1997046243A1 (en) * | 1996-06-04 | 1997-12-11 | The Procter & Gamble Company | A nasal spray containing an intranasal steroid and an antihistamine |
US6319513B1 (en) * | 1998-08-24 | 2001-11-20 | The Procter & Gamble Company | Oral liquid mucoadhesive compounds |
US6793942B2 (en) * | 2000-02-23 | 2004-09-21 | Bioselect Innovations, Inc. | Composition and method for treating the effects of diseases and maladies |
AU2006226887A1 (en) * | 2005-03-23 | 2006-09-28 | Elan Pharma International Limited | Nanoparticulate corticosteroid and antihistamine formulations |
US20080058421A1 (en) * | 2006-09-05 | 2008-03-06 | John Alex Lopes | Compositions for cleaning and disinfecting nasal tract and sinus cavity |
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2020
- 2020-02-14 WO PCT/US2020/018430 patent/WO2020168289A1/en active Application Filing
- 2020-02-14 EP EP20754134.3A patent/EP3965886A4/en active Pending
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